Pub Date : 2024-03-12DOI: 10.2174/0115734072297243240304113132
Afaf Chebout, M. Chaalal, S. Ydjedd, Louiza Himed
The encapsulation technique is an effective method for coating bioactive molecules and protecting them against various technological treatment conditions during production processing. The aim of this study was to optimize the encapsulation conditions of phenolic compounds extracted from Malabar nut (Justicia adhatoda L.) leaves by alginate emulsion-gelation approach using response surface methodology The ionotropic gelation method was used to encapsulate the phenolic compounds of Malabar nut (Justicia adhatoda L.) leaves. The optimization of this phenolic compounds encapsulation was carried out using response surface methodology through Box˗Behnken design. Four parameters with three levels (-1, 0, +1) were chosen including sodium alginate concentration (2 – 3 - 4%), calcium chloride concentration (4 - 6 - 8%), plant extract-alginate solution ratio (0.02 – 0.11 - 0.2 mg/ml), and gelation time (5 – 12.5 - 20 min). of the total phenolic and flavonoid contents encapsulation efficiency was assessed. Likewise, the antioxidant activity was evaluated using ferric-reducing power (FRP) and free radical scavenging activity (DPPH). The results of response surface methodology analysis using Box˗Behnken design showed that the optimal encapsulation conditions were 3.11% for alginate concentration, 5.74% for calcium chloride concentration, 0.1 mg/ml for the plant extract-alginate solution ratio, and 10.80 min for gelation time. Under these conditions, the optimum values of total phenolic and flavonoid encapsulation efficiency were 86.17% and 75.69%, respectively, 126.75 mg AAE/100 g for ferric reducing power and 97.29% for DPPH. The experimental and prediction results have expressed a high significant level for all responses. The method revealed the validity of elaborated models through response surface methodology optimization processes for phenolic antioxidants encapsulation of Malabar nut (Justicia adhatoda L.) leaves extract.
{"title":"Optimization of Malabar Nut (Justicia adhatoda L.) Leaves’ Phenolic\u0000Compounds by Alginate Emulsion-gelation Approach using Response\u0000Surface Methodology","authors":"Afaf Chebout, M. Chaalal, S. Ydjedd, Louiza Himed","doi":"10.2174/0115734072297243240304113132","DOIUrl":"https://doi.org/10.2174/0115734072297243240304113132","url":null,"abstract":"\u0000\u0000The encapsulation technique is an effective method for coating bioactive\u0000molecules and protecting them against various technological treatment conditions during production processing.\u0000\u0000\u0000\u0000The aim of this study was to optimize the encapsulation conditions of phenolic compounds extracted from Malabar nut (Justicia adhatoda L.) leaves by alginate emulsion-gelation\u0000approach using response surface methodology\u0000\u0000\u0000\u0000The ionotropic gelation method was used to encapsulate the phenolic compounds of\u0000Malabar nut (Justicia adhatoda L.) leaves. The optimization of this phenolic compounds encapsulation was carried out using response surface methodology through Box˗Behnken design. Four\u0000parameters with three levels (-1, 0, +1) were chosen including sodium alginate concentration\u0000(2 – 3 - 4%), calcium chloride concentration (4 - 6 - 8%), plant extract-alginate solution ratio\u0000(0.02 – 0.11 - 0.2 mg/ml), and gelation time (5 – 12.5 - 20 min). of the total phenolic and flavonoid contents encapsulation efficiency was assessed. Likewise, the antioxidant activity was evaluated using ferric-reducing power (FRP) and free radical scavenging activity (DPPH).\u0000\u0000\u0000\u0000The results of response surface methodology analysis using Box˗Behnken design\u0000showed that the optimal encapsulation conditions were 3.11% for alginate concentration, 5.74%\u0000for calcium chloride concentration, 0.1 mg/ml for the plant extract-alginate solution ratio, and\u000010.80 min for gelation time. Under these conditions, the optimum values of total phenolic and\u0000flavonoid encapsulation efficiency were 86.17% and 75.69%, respectively, 126.75 mg AAE/100\u0000g for ferric reducing power and 97.29% for DPPH. The experimental and prediction results have\u0000expressed a high significant level for all responses.\u0000\u0000\u0000\u0000The method revealed the validity of elaborated models through response surface\u0000methodology optimization processes for phenolic antioxidants encapsulation of Malabar nut\u0000(Justicia adhatoda L.) leaves extract.\u0000","PeriodicalId":10772,"journal":{"name":"Current Bioactive Compounds","volume":"7 6","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-03-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140248582","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2024-03-05DOI: 10.2174/0115734072296125240221061200
K. Gaur, Y. Siddique
Environmental pollutants pose a serious risk to human health and are a factor in the emergence of many diseases and disorders. In recent years, the research for efficient defence against these pollutants has focused much interest. Natural flavonoid apigenin in various fruits and vegetables has shown great defence against environmental toxins. This review aims to summarize the current knowledge regarding the protective effect of apigenin environmental pollutants and its underlying mechanisms. The study starts by summarizing the main industrial chemicals, environmental pollutants, water contaminants, and the health hazards they provide. The article discusses apigenin's bioactive attributes and focuses on its anti-inflammatory, detoxifying, and antioxidant activities. Previous studies have shown that apigenin supplementation can reduce oxidative stress, inflammation, DNA damage, and organ toxicity from pollutants. The molecular processes behind apigenin's anti-inflammatory effects are explored, including its interactions with important signaling networks. Additional research is required to assess its ideal dosage, bioavailability, and potential interactions with other drugs. Moreover, more human studies are required to evaluate the long-term advantages and safety of apigenin supplementation as a defence against the harmful health consequences of environmental contaminants.
{"title":"The Role of Apigenin in Alleviating the Impact of Environmental Pollutants","authors":"K. Gaur, Y. Siddique","doi":"10.2174/0115734072296125240221061200","DOIUrl":"https://doi.org/10.2174/0115734072296125240221061200","url":null,"abstract":"\u0000\u0000Environmental pollutants pose a serious risk to human health and are a factor in the\u0000emergence of many diseases and disorders. In recent years, the research for efficient defence\u0000against these pollutants has focused much interest. Natural flavonoid apigenin in various fruits\u0000and vegetables has shown great defence against environmental toxins. This review aims to summarize\u0000the current knowledge regarding the protective effect of apigenin environmental pollutants\u0000and its underlying mechanisms. The study starts by summarizing the main industrial chemicals,\u0000environmental pollutants, water contaminants, and the health hazards they provide. The article\u0000discusses apigenin's bioactive attributes and focuses on its anti-inflammatory, detoxifying, and\u0000antioxidant activities. Previous studies have shown that apigenin supplementation can reduce oxidative\u0000stress, inflammation, DNA damage, and organ toxicity from pollutants. The molecular\u0000processes behind apigenin's anti-inflammatory effects are explored, including its interactions with\u0000important signaling networks. Additional research is required to assess its ideal dosage, bioavailability,\u0000and potential interactions with other drugs. Moreover, more human studies are required to\u0000evaluate the long-term advantages and safety of apigenin supplementation as a defence against\u0000the harmful health consequences of environmental contaminants.\u0000","PeriodicalId":10772,"journal":{"name":"Current Bioactive Compounds","volume":"45 2","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-03-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140264464","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2024-03-04DOI: 10.2174/0115734072287039240214112330
Salima Djafri-Dib, Yalaoui-Guellal Drifa, N. Amessis-Ouchemoukh, K. Madani, S. Ouchemoukh
Biosurfactants are very important amphiphile compounds due to their interesting advantages such as low toxicity, biodegradability and also their many biological properties. In the present study, antimicrobial and anti-imflammatory activities were evaluated to determine the biological proprieties of biosurfactant BLA 2906 produced by Alcaligenes aquatilis YGD 2906 using different assays. Screening and optimization component concentrations in the medium were investigated using PBD and SRM to increase surfactant yield in term emulsification activity value (E24%). The halos of antifungal activity presented a mean value of 12.33 mm to 17.67 mm. For antibacterial activity, the diameter varied from 10.33 to 12.67 mm with a very important antiinflammatory activity using a protein denaturation method that showed a maximum inhibition of 92.79%. These results suggest that BLA 2906 may be used as a new therapeutic and antiinflammatory agent. The PBD selected 7 significant components out of the 14 screened. The RSM resulted in the production in terms of emulsification activity of 68.37% in the optimized medium.
{"title":"Optimization of Lipopeptide Biosurfactant Production with\u0000Anti-Inflammatory and Antimicrobial Activities","authors":"Salima Djafri-Dib, Yalaoui-Guellal Drifa, N. Amessis-Ouchemoukh, K. Madani, S. Ouchemoukh","doi":"10.2174/0115734072287039240214112330","DOIUrl":"https://doi.org/10.2174/0115734072287039240214112330","url":null,"abstract":"\u0000\u0000Biosurfactants are very important amphiphile compounds due to their\u0000interesting advantages such as low toxicity, biodegradability and also their many biological properties.\u0000\u0000\u0000\u0000In the present study, antimicrobial and anti-imflammatory activities were evaluated to\u0000determine the biological proprieties of biosurfactant BLA 2906 produced by Alcaligenes aquatilis\u0000YGD 2906 using different assays. Screening and optimization component concentrations in the\u0000medium were investigated using PBD and SRM to increase surfactant yield in term emulsification\u0000activity value (E24%).\u0000\u0000\u0000\u0000The halos of antifungal activity presented a mean value of 12.33 mm to 17.67 mm. For\u0000antibacterial activity, the diameter varied from 10.33 to 12.67 mm with a very important antiinflammatory\u0000activity using a protein denaturation method that showed a maximum inhibition of\u000092.79%.\u0000\u0000\u0000\u0000These results suggest that BLA 2906 may be used as a new therapeutic and antiinflammatory\u0000agent. The PBD selected 7 significant components out of the 14 screened. The\u0000RSM resulted in the production in terms of emulsification activity of 68.37% in the optimized\u0000medium.\u0000","PeriodicalId":10772,"journal":{"name":"Current Bioactive Compounds","volume":"9 4","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-03-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140266315","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
The constant increase in global onion production escalates the generation of onion peel waste. For instance, globally, >50 lakh tons of onion waste are generated annually. Its objectionable odor precludes its use in agriculture or disposal as landfilling presents environmental issues. Previous studies show that two major flavonoids, quercetin and its glycosides (spiraeoside), have been identified in abundance in onion waste. By utilizing the spiraeoside (quercetin-4ʹ-glucoside), a rapid synthesis of pachypodol (quercetin-3,3′,7-trimethyl ether, and a rare flavonol), an essential Ayurvedic product, has been developed and achieved. Pachypodol and analogs were studied for their ability to inhibit matrix metalloproteinase-2 and -9 (MMP-2 & 9) activity. Amongst the compounds tested, pachypodol significantly inhibited MMP-2 activity. In-silico docking studies suggest that, unlike most known MMP inhibitors, pachypodol interacts selectively with MMP-2 through the residues Ile222, Tyr223, and Thr227 in a zincindependent manner. The experimental studies also prove that pachypodol inhibits the MMP-2 enzyme in a zinc-independent way.
{"title":"Probing Anticancer Molecules from Onion Peels Waste; First Synthesis and Biological Studies of a Rare Quercetin Derivative-Pachypodol","authors":"Pandurangan Nanjan, Jyotsna Nambiar, Chinchu Bose, Asoke Banerji, Bipin G. Nair","doi":"10.2174/0115734072293689240219110806","DOIUrl":"https://doi.org/10.2174/0115734072293689240219110806","url":null,"abstract":"\u0000\u0000The constant increase in global onion production escalates the generation\u0000of onion peel waste. For instance, globally, >50 lakh tons of onion waste are generated annually.\u0000\u0000\u0000\u0000Its objectionable odor precludes its use in agriculture or disposal as landfilling presents\u0000environmental issues. Previous studies show that two major flavonoids, quercetin and its glycosides\u0000(spiraeoside), have been identified in abundance in onion waste. By utilizing the spiraeoside\u0000(quercetin-4ʹ-glucoside), a rapid synthesis of pachypodol (quercetin-3,3′,7-trimethyl ether, and a\u0000rare flavonol), an essential Ayurvedic product, has been developed and achieved. Pachypodol and\u0000analogs were studied for their ability to inhibit matrix metalloproteinase-2 and -9 (MMP-2 & 9)\u0000activity. Amongst the compounds tested, pachypodol significantly inhibited MMP-2 activity.\u0000\u0000\u0000\u0000In-silico docking studies suggest that, unlike most known MMP inhibitors, pachypodol\u0000interacts selectively with MMP-2 through the residues Ile222, Tyr223, and Thr227 in a zincindependent\u0000manner.\u0000\u0000\u0000\u0000The experimental studies also prove that pachypodol inhibits the MMP-2 enzyme in\u0000a zinc-independent way.\u0000","PeriodicalId":10772,"journal":{"name":"Current Bioactive Compounds","volume":"84 3","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140084862","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2024-02-23DOI: 10.2174/0115734072275742240103055511
A. Chettupalli, P. R. Amarachinta, Mounika Kuchukuntla, Sunand Katta, Vijay Kumar Vobenaboina, Baba Shankar Rao Garige, Pranay Renukuntla, L. Samein
Nimodipine is a highly lipophilic anti-hypertensive drug having 13% oral bioavailability (log P 3.41). Nimodipine is a prominent calcium channel blocker that must be given intravenously for an extended period of time (1-2 weeks) in order to treat cerebral vasospasm. It might be possible to substitute a sustained-release biodegradable formulation for the ongoing intravenous infusion used in this traditional therapy. The primary goal of this study was to formulate and evaluate the potentiality of ethosomes to deliver nimodipine, a potent water-insoluble anti-hypertensive drug, through the deeper layers of the skin. The greatest challenge for drug formulation is its poor oral bioavailability and solubility. Nimodipine-loaded ethosomal gel was developed for transdermal drug delivery to increase solubility and skin penetration and to promote oral bioavailability. Central composite design employing a thin-film hydration method was used to prepare and optimize ethosomes. A better dispersion medium for nimodipine's preparation in ethosomes was selected based on the effect. The design consisted of independent variables as lipid (X1), ethanol (X2), and sonication time (X3). Concentrations were manipulated to examine the effects on three responses, namely the %entrapment efficiency (Y1), vesicle size (Y2), and %cumulative drug release (Y3). Surface morphology and other in vitro tests were used to identify ethosomes containing nimodipine. The preparation of ethosomal gel formulations began with incorporating a single ethosomal formulation (F4) into various concentrations of gelling agents. These studies performed physicochemical characterization, compatibility testing, and in vitro drug release tests on ethosomal gels. In vivo studies involving hypertensive rats were conducted after skin permeation, and ex vivo studies were performed. In order to assess the drug's permeability and deposition, we employed the abdomen skin of rats. The optimal process parameters resulted in ethosomes with 89.9 ± 0.19 percent entrapment efficiency, a vesicle size of 102.37 ± 5.84 nm, and a cumulative drug release of 98.3 ± 0.13%. pH and drug content measurements were consistent with the homogeneous ethosomal gels. Viscosity was found to increase with the spreadability. The ethosomal gel formulation (G2) met the regulatory standards regarding appearance, spreadability, viscosity, and in vitro release studies. Compared to pure nimodipine, ethosomal suspension (F4) and ethosomal gel (G2) formulations had higher ex vivo permeation, steady-state flux, and drug retention. Rats' mean arterial pressure (146.11 ± 0.84 mmHg) was significantly lower (p < 0.01) after after two hours of the experiment than it had been (p < 0.001) (98.88 ± 0.63 mmHg) after six hours. To summarize, ethosomal gels have been found to be lipid carriers that enhance skin permeation and extend the anti-hypertensive effect of nimodipine. Compared to plain gel, ex vivo drug permeation through rat abdom
{"title":"Quality by Design and Characterization of Nimodipine Novel Carriers for the Treatment of Hypertension: Assessment of the Pharmacokinetic Profile","authors":"A. Chettupalli, P. R. Amarachinta, Mounika Kuchukuntla, Sunand Katta, Vijay Kumar Vobenaboina, Baba Shankar Rao Garige, Pranay Renukuntla, L. Samein","doi":"10.2174/0115734072275742240103055511","DOIUrl":"https://doi.org/10.2174/0115734072275742240103055511","url":null,"abstract":"\u0000\u0000Nimodipine is a highly lipophilic anti-hypertensive drug having 13%\u0000oral bioavailability (log P 3.41). Nimodipine is a prominent calcium channel blocker that must be\u0000given intravenously for an extended period of time (1-2 weeks) in order to treat cerebral vasospasm.\u0000It might be possible to substitute a sustained-release biodegradable formulation for the\u0000ongoing intravenous infusion used in this traditional therapy.\u0000\u0000\u0000\u0000The primary goal of this study was to formulate and evaluate the potentiality of ethosomes\u0000to deliver nimodipine, a potent water-insoluble anti-hypertensive drug, through the deeper layers of the\u0000skin. The greatest challenge for drug formulation is its poor oral bioavailability and solubility.\u0000\u0000\u0000\u0000Nimodipine-loaded ethosomal gel was developed for transdermal drug delivery to increase\u0000solubility and skin penetration and to promote oral bioavailability. Central composite design\u0000employing a thin-film hydration method was used to prepare and optimize ethosomes. A better\u0000dispersion medium for nimodipine's preparation in ethosomes was selected based on the effect. The\u0000design consisted of independent variables as lipid (X1), ethanol (X2), and sonication time (X3).\u0000Concentrations were manipulated to examine the effects on three responses, namely the %entrapment\u0000efficiency (Y1), vesicle size (Y2), and %cumulative drug release (Y3). Surface morphology\u0000and other in vitro tests were used to identify ethosomes containing nimodipine. The preparation of\u0000ethosomal gel formulations began with incorporating a single ethosomal formulation (F4) into various\u0000concentrations of gelling agents. These studies performed physicochemical characterization,\u0000compatibility testing, and in vitro drug release tests on ethosomal gels. In vivo studies involving hypertensive\u0000rats were conducted after skin permeation, and ex vivo studies were performed. In order\u0000to assess the drug's permeability and deposition, we employed the abdomen skin of rats.\u0000\u0000\u0000\u0000The optimal process parameters resulted in ethosomes with 89.9 ± 0.19 percent entrapment\u0000efficiency, a vesicle size of 102.37 ± 5.84 nm, and a cumulative drug release of 98.3 ±\u00000.13%. pH and drug content measurements were consistent with the homogeneous ethosomal\u0000gels. Viscosity was found to increase with the spreadability. The ethosomal gel formulation (G2)\u0000met the regulatory standards regarding appearance, spreadability, viscosity, and in vitro release\u0000studies. Compared to pure nimodipine, ethosomal suspension (F4) and ethosomal gel (G2) formulations\u0000had higher ex vivo permeation, steady-state flux, and drug retention. Rats' mean arterial\u0000pressure (146.11 ± 0.84 mmHg) was significantly lower (p < 0.01) after after two hours of the\u0000experiment than it had been (p < 0.001) (98.88 ± 0.63 mmHg) after six hours.\u0000\u0000\u0000\u0000To summarize, ethosomal gels have been found to be lipid carriers that enhance skin\u0000permeation and extend the anti-hypertensive effect of nimodipine. Compared to plain gel, ex vivo\u0000drug permeation through rat abdom","PeriodicalId":10772,"journal":{"name":"Current Bioactive Compounds","volume":"62 5","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-02-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140436923","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2024-02-22DOI: 10.2174/0115734072282575240213091008
Kaushal Arora, Amit Kumar, P. Verma
A new series of 2-(2-(substituted aldehyde)hydrazinyl)-4-(2- chlorophenyl)-1-methyl-6-oxo-1,6-dihydropyrimidine-5-carbonitrile analogs (1–19) was prepared by using the Biginelli reaction. A novel series of 2-(2-(substituted aldehyde)hydrazinyl)-4-(2-chlorophenyl)-1-methyl-6-oxo-1,6-dihydropyrimidine-5-carbonitrile analogues (1–19) was synthesized using the Biginelli reaction TLC was employed to ensure the progress and confirmation of the reactions. Silica gel G was employed as the stationary phase, and mobile phases such as chloroform: toluene and acetone: n-hexane were used for the synthesized compounds. NMR has characterized the synthesized compound. MS IR, CHN. The prepared derivatives were evaluated in vitro for antimicrobial activity against various bacteria and fungi using the tube dilution technique. Notably, compounds 2-(2-(3-Ethoxy-4- hydroxybenzylidene)hydrazinyl)-4-(2-chlorophenyl)-1-methyl-6-oxo-1,6-dihydropyrimidine-5- carbonitrile T1, 2-(2-(2-Hydroxybenzylidene)hydrazinyl)-4-(2-chlorophenyl)-1-methyl-6-oxo-1,6- dihydropyrimidine-5 carbonitrile T6, and 2-(2-(4-Hydroxybenzylidene)hydrazinyl)-4-(2- chlorophenyl)-1-methyl-6-oxo-1,6-dihydropyrimidine-5-carbonitrile T16, displayed significant antibacterial activity, surpassing the standard drug Ampicillin. In the antifungal category, compounds 2-(2-(3-Ethoxy-4-hydroxybenzylidene)hydrazinyl)-4-(2-chlorophenyl)-1-methyl-6-oxo-1,6-dihydropyri midine-5-carbonitrile T1, 2-(2-(3,4-Dimethoxybenzylidene)hydrazinyl)-4-(2-chlorophenyl)-1-methyl-6- oxo-1,6-dihydropyrimidine-5-carbonitrile T2, and 2-(2-(2,4-Dichlorobenzylidene)hydrazinyl)-4-(2- chlorophenyl)-1-methyl-6-oxo-1,6-dihydropyrimidine-5-carbonitrile T13, were very much effective against both fungal strains A. niger as well as C. albicans. Furthermore, compounds 2-(2-(2- Hydroxybenzylidene)hydrazinyl)-4-(2-chlorophenyl)-1-methyl-6-oxo-1,6-dihydropyrimidine-5 carbonitrile T6, 2-(2-(2-Nitrobenzylidene)hydrazinyl)-4-(2-chlorophenyl)-1-methyl-6-oxo-1,6-dihydropyri midine-5-carbonitrile T8, 2-(2-(4-Chlorobenzylidene)hydrazinyl)-4-(2-chlorophenyl)-1-methyl-6-oxo- 1,6-dihydropyrimidine-5-carbonitrile T12, and 2-(2-(4-Dimethylaminobenzylidene)hydrazinyl)-4-(2- chlorophenyl)-1-methyl-6-oxo-1,6-dihydropyrimidine-5-carbonitrile T14 demonstrated remarkable antioxidant properties, because of their low IC50 values in the DPPH assay. In the realm of anticancer activity, 2-(2-(substituted aldehyde)hydrazinyl)-4-(2-chlorophenyl)-1-methyl-6-oxo-1,6-dihydro pyrimidine-5-carbonitrile T9 outperformed the standard drug Adriamycin in terms of its effectiveness against human lung cancer cells (A-549) with a GI50 value of less than 10 according to the SRB assay. In addition, the antidiabetic assessment highlighted the excellent performance of compounds 2-(2- (2-Nitrobenzylidene)hydrazinyl)-4-(2-chlorophenyl)-1-methyl-6-oxo-1,6-dihydropyrimidine-5- carbonitrile T8, 2-(2-(4-Chlorobenzylidene)hydrazinyl)-4-(2-chlorophenyl)-1-methyl-6-oxo-1,6- dihydropyrimidi
{"title":"A Convenient and Practical Synthesis of Novel Pyrimidine Derivatives and\u0000its Therapeutic Potential","authors":"Kaushal Arora, Amit Kumar, P. Verma","doi":"10.2174/0115734072282575240213091008","DOIUrl":"https://doi.org/10.2174/0115734072282575240213091008","url":null,"abstract":"\u0000\u0000A new series of 2-(2-(substituted aldehyde)hydrazinyl)-4-(2-\u0000chlorophenyl)-1-methyl-6-oxo-1,6-dihydropyrimidine-5-carbonitrile analogs (1–19) was prepared\u0000by using the Biginelli reaction.\u0000\u0000\u0000\u0000A novel series of 2-(2-(substituted aldehyde)hydrazinyl)-4-(2-chlorophenyl)-1-methyl-6-oxo-1,6-dihydropyrimidine-5-carbonitrile analogues (1–19) was synthesized using the Biginelli reaction\u0000\u0000\u0000\u0000TLC was employed to ensure the progress and confirmation of the reactions. Silica gel\u0000G was employed as the stationary phase, and mobile phases such as chloroform: toluene and acetone:\u0000n-hexane were used for the synthesized compounds. NMR has characterized the synthesized\u0000compound. MS IR, CHN.\u0000\u0000\u0000\u0000The prepared derivatives were evaluated in vitro for antimicrobial activity against various\u0000bacteria and fungi using the tube dilution technique. Notably, compounds 2-(2-(3-Ethoxy-4-\u0000hydroxybenzylidene)hydrazinyl)-4-(2-chlorophenyl)-1-methyl-6-oxo-1,6-dihydropyrimidine-5-\u0000carbonitrile T1, 2-(2-(2-Hydroxybenzylidene)hydrazinyl)-4-(2-chlorophenyl)-1-methyl-6-oxo-1,6-\u0000dihydropyrimidine-5 carbonitrile T6, and 2-(2-(4-Hydroxybenzylidene)hydrazinyl)-4-(2-\u0000chlorophenyl)-1-methyl-6-oxo-1,6-dihydropyrimidine-5-carbonitrile T16, displayed significant\u0000antibacterial activity, surpassing the standard drug Ampicillin. In the antifungal category, compounds\u00002-(2-(3-Ethoxy-4-hydroxybenzylidene)hydrazinyl)-4-(2-chlorophenyl)-1-methyl-6-oxo-1,6-dihydropyri\u0000midine-5-carbonitrile T1, 2-(2-(3,4-Dimethoxybenzylidene)hydrazinyl)-4-(2-chlorophenyl)-1-methyl-6-\u0000oxo-1,6-dihydropyrimidine-5-carbonitrile T2, and 2-(2-(2,4-Dichlorobenzylidene)hydrazinyl)-4-(2-\u0000chlorophenyl)-1-methyl-6-oxo-1,6-dihydropyrimidine-5-carbonitrile T13, were very much effective\u0000against both fungal strains A. niger as well as C. albicans. Furthermore, compounds 2-(2-(2-\u0000Hydroxybenzylidene)hydrazinyl)-4-(2-chlorophenyl)-1-methyl-6-oxo-1,6-dihydropyrimidine-5 carbonitrile\u0000T6, 2-(2-(2-Nitrobenzylidene)hydrazinyl)-4-(2-chlorophenyl)-1-methyl-6-oxo-1,6-dihydropyri\u0000midine-5-carbonitrile T8, 2-(2-(4-Chlorobenzylidene)hydrazinyl)-4-(2-chlorophenyl)-1-methyl-6-oxo-\u00001,6-dihydropyrimidine-5-carbonitrile T12, and 2-(2-(4-Dimethylaminobenzylidene)hydrazinyl)-4-(2-\u0000chlorophenyl)-1-methyl-6-oxo-1,6-dihydropyrimidine-5-carbonitrile T14 demonstrated remarkable\u0000antioxidant properties, because of their low IC50 values in the DPPH assay. In the realm of anticancer\u0000activity, 2-(2-(substituted aldehyde)hydrazinyl)-4-(2-chlorophenyl)-1-methyl-6-oxo-1,6-dihydro\u0000pyrimidine-5-carbonitrile T9 outperformed the standard drug Adriamycin in terms of its effectiveness\u0000against human lung cancer cells (A-549) with a GI50 value of less than 10 according to the SRB assay.\u0000In addition, the antidiabetic assessment highlighted the excellent performance of compounds 2-(2-\u0000(2-Nitrobenzylidene)hydrazinyl)-4-(2-chlorophenyl)-1-methyl-6-oxo-1,6-dihydropyrimidine-5-\u0000carbonitrile T8, 2-(2-(4-Chlorobenzylidene)hydrazinyl)-4-(2-chlorophenyl)-1-methyl-6-oxo-1,6-\u0000dihydropyrimidi","PeriodicalId":10772,"journal":{"name":"Current Bioactive Compounds","volume":"25 15","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-02-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140441836","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
By condensing 2-aminothiazole and phenacyl bromide, a novel catalystfree synthetic approach for the synthesis of imidazo[2,1-b]thiazole derivatives has been developed. In this work, aloe vera/water (3:2) is used as a reusable, environmentally benign, greenpromoting media to synthesize desired products. This method enables the synthesis of a diverse range of aryl-substituted imidazo[2,1-b]thiazoles. This solvent system demonstrates remarkable efficiency and offers numerous advantages, including shorter reaction times, the absence of side product formation, costeffectiveness, excellent atom efficiency, straightforward operation, and high yields. In conclusion, we successfully developed a green protocol for the environmentally benign synthesis of imidazo[2,1-b]thiazole derivatives using aloe vera water as green-promoting media.
{"title":"Catalyst-free Aloe Vera-promoted Cyclization of 2-Amino-azarenes with Phenacyl Bromide","authors":"Jyoti Baranwal, Swastika Singh, Smriti Kushwaha, Archana Jyoti","doi":"10.2174/0115734072278083240214060120","DOIUrl":"https://doi.org/10.2174/0115734072278083240214060120","url":null,"abstract":"\u0000\u0000By condensing 2-aminothiazole and phenacyl bromide, a novel catalystfree\u0000synthetic approach for the synthesis of imidazo[2,1-b]thiazole derivatives has been developed.\u0000\u0000\u0000\u0000In this work, aloe vera/water (3:2) is used as a reusable, environmentally benign, greenpromoting\u0000media to synthesize desired products. This method enables the synthesis of a diverse\u0000range of aryl-substituted imidazo[2,1-b]thiazoles.\u0000\u0000\u0000\u0000This solvent system demonstrates remarkable efficiency and offers numerous advantages,\u0000including shorter reaction times, the absence of side product formation, costeffectiveness,\u0000excellent atom efficiency, straightforward operation, and high yields.\u0000\u0000\u0000\u0000In conclusion, we successfully developed a green protocol for the environmentally\u0000benign synthesis of imidazo[2,1-b]thiazole derivatives using aloe vera water as green-promoting\u0000media.\u0000","PeriodicalId":10772,"journal":{"name":"Current Bioactive Compounds","volume":"98 3","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-02-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140438212","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2024-02-21DOI: 10.2174/0115734072284841240207104403
Himanchal Sharma, Divya Pathak, Sachin Kumar
Alkaloids are nitrogen-containing chemical compounds found in nature. Many alkaloids are heterocyclic in nature. They are nitrogen-based organic compounds with the nitrogen atoms enclosed in a heterocyclic ring. The chemical "pro alkaloid" is derived from the alkyl amines in it. Many ancient people, long before the advent of organic chemistry, recognized that many of these substances have measurable effects on the body's physiological functions. Alkaloids are a type of natural substances that are classified as secondary metabolites. Many different types of organisms create alkaloids, which are a class of natural products. Alkaloids showed antifungal, local anesthetic, anti-inflammatory, anticancer, analgesic, neuropharmacologic, antimicrobial, and many other activities. Amines, as opposed to alkaloids, are the more common classification for naturally occurring compounds that contain nitrogen in the exocyclic position (such as mescaline, serotonin, and dopamine). An amide molecule has a nitrogen atom that is chemically bound to a carbon atom in the carbonyl group. The -oic acid ending of the corresponding carboxylic acid is converted to -amide to form the correct nomenclature for an amide. This article offers an overview of numerous techniques for extracting, separating, and purifying alkaloids for use in natural medicine.
{"title":"Recent Progress in Isolating and Purifying Amide Alkaloids from their\u0000Natural Habitats: A Review","authors":"Himanchal Sharma, Divya Pathak, Sachin Kumar","doi":"10.2174/0115734072284841240207104403","DOIUrl":"https://doi.org/10.2174/0115734072284841240207104403","url":null,"abstract":"\u0000\u0000Alkaloids are nitrogen-containing chemical compounds found in nature. Many alkaloids\u0000are heterocyclic in nature. They are nitrogen-based organic compounds with the nitrogen\u0000atoms enclosed in a heterocyclic ring. The chemical \"pro alkaloid\" is derived from the alkyl\u0000amines in it. Many ancient people, long before the advent of organic chemistry, recognized that\u0000many of these substances have measurable effects on the body's physiological functions. Alkaloids\u0000are a type of natural substances that are classified as secondary metabolites. Many different\u0000types of organisms create alkaloids, which are a class of natural products. Alkaloids showed antifungal,\u0000local anesthetic, anti-inflammatory, anticancer, analgesic, neuropharmacologic, antimicrobial,\u0000and many other activities. Amines, as opposed to alkaloids, are the more common classification\u0000for naturally occurring compounds that contain nitrogen in the exocyclic position (such\u0000as mescaline, serotonin, and dopamine). An amide molecule has a nitrogen atom that is chemically\u0000bound to a carbon atom in the carbonyl group. The -oic acid ending of the corresponding carboxylic\u0000acid is converted to -amide to form the correct nomenclature for an amide. This article\u0000offers an overview of numerous techniques for extracting, separating, and purifying alkaloids for\u0000use in natural medicine.\u0000","PeriodicalId":10772,"journal":{"name":"Current Bioactive Compounds","volume":"150 4","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-02-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140443820","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2024-02-15DOI: 10.2174/0115734072282832240122020523
D. Foda, Heba-tollah M. Sweelam, Noha E. Ibrahim
Rosmarinus officinalis is considered one of the famous plants from ancient times for its therapeutic ability in many diseases, such as headache, spasms, brain disorders, and some pathological conditions associated with toxicity cases in the liver and kidneys. The current research has aimed, for the first time, to evaluate anti-urolithiatic effect of Rosmarinus officinalis aqueous extract (RMAE) on calcium oxalate stones formation in male rats and its possible therapeutic mechanisms of action. Evaluation of the polyphenols and flavonoid content in the extract was also performed. A calcium oxalate nephrolithiasis case was established in rats by adding ethylene glycol (1%) to the rats' daily drinking water for a duration of one month. Treatment was achieved by oral co-administration of RMAE to rats administrated ethylene glycol. Phytochemical results showed that LC/MS-MS analysis led to the identification of 37 compounds in the phytoconstituent profile of RMAE. The biochemical results revealed significant improvement in serum kidney functions (urea, creatinine, and uric acid) in addition to restoring the calcium x phosphorous product and parathyroid hormone (PTH) levels in the plant-treated group compared to the non-treated one. The data have been supported by the significant decrease in lactate dehydrogenase enzyme (LDH) expression in the liver tissues, reflecting the decrease in oxalate synthesis in the liver compared to the non-treated group. Kidneys' histological examinations showed the absence of oxalate crystals in the treated group and the immunohistochemical findings of osteopontin (OPN) protein revealed the impact of RMAE on OPN expression in kidney tissues. Improvements in the femur bone fractures and the parathyroid gland in the treated group were also noticed during microscopic examinations. The anti-lithiatic effect of the extract was attributed to its influence on serum phosphate, serum PTH, and OPN levels in kidney tissues and decreasing synthesis of LDH in liver tissues in addition to the prevention of secondary disease incidences, such as secondary hyperparathyroidism and cardiovascular diseases. On the other hand, the plant's considerable content of phenolics and flavonoids has been found to play a role in controlling kidney stone progression episodes.
{"title":"Role of Rosmarinus officinalis Aqueous Extract in Relieving the Complications\u0000Associated with Ethylene Glycol-induced Urolithiasis in Male Rats","authors":"D. Foda, Heba-tollah M. Sweelam, Noha E. Ibrahim","doi":"10.2174/0115734072282832240122020523","DOIUrl":"https://doi.org/10.2174/0115734072282832240122020523","url":null,"abstract":"\u0000\u0000Rosmarinus officinalis is considered one of the famous plants from ancient\u0000times for its therapeutic ability in many diseases, such as headache, spasms, brain disorders,\u0000and some pathological conditions associated with toxicity cases in the liver and kidneys.\u0000\u0000\u0000\u0000The current research has aimed, for the first time, to evaluate anti-urolithiatic effect of Rosmarinus\u0000officinalis aqueous extract (RMAE) on calcium oxalate stones formation in male rats and\u0000its possible therapeutic mechanisms of action. Evaluation of the polyphenols and flavonoid content\u0000in the extract was also performed.\u0000\u0000\u0000\u0000A calcium oxalate nephrolithiasis case was established in rats by adding ethylene glycol\u0000(1%) to the rats' daily drinking water for a duration of one month. Treatment was achieved by\u0000oral co-administration of RMAE to rats administrated ethylene glycol.\u0000\u0000\u0000\u0000Phytochemical results showed that LC/MS-MS analysis led to the identification of 37\u0000compounds in the phytoconstituent profile of RMAE. The biochemical results revealed significant\u0000improvement in serum kidney functions (urea, creatinine, and uric acid) in addition to restoring\u0000the calcium x phosphorous product and parathyroid hormone (PTH) levels in the plant-treated\u0000group compared to the non-treated one. The data have been supported by the significant decrease\u0000in lactate dehydrogenase enzyme (LDH) expression in the liver tissues, reflecting the decrease in\u0000oxalate synthesis in the liver compared to the non-treated group. Kidneys' histological examinations\u0000showed the absence of oxalate crystals in the treated group and the immunohistochemical\u0000findings of osteopontin (OPN) protein revealed the impact of RMAE on OPN expression in kidney\u0000tissues. Improvements in the femur bone fractures and the parathyroid gland in the treated\u0000group were also noticed during microscopic examinations.\u0000\u0000\u0000\u0000The anti-lithiatic effect of the extract was attributed to its influence on serum phosphate,\u0000serum PTH, and OPN levels in kidney tissues and decreasing synthesis of LDH in liver\u0000tissues in addition to the prevention of secondary disease incidences, such as secondary hyperparathyroidism\u0000and cardiovascular diseases. On the other hand, the plant's considerable content\u0000of phenolics and flavonoids has been found to play a role in controlling kidney stone progression\u0000episodes.\u0000","PeriodicalId":10772,"journal":{"name":"Current Bioactive Compounds","volume":"23 6","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-02-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139963355","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2024-02-15DOI: 10.2174/0115734072294929240206060527
Sasmita Dash, Nityananda Sahoo, G. Pattnaik, Chandan Das, Sovan Pattnaik, Goutam Ghosh, Goutam Rath, B. Kar
Diabetes mellitus (DM) is a metabolic disorder caused by insufficient insulin production from pancreatic β-cells or insulin resistance; its prevalence rapidly increases worldwide. Increasing reports indicate that most plant bioactive agents exhibited alternative and safe effects in managing DM. The study aims to evaluate the in vitro antioxidant and anti-diabetic efficacy of the combination of Annona squamosa Linn. (AS) leaf extract and Oleanolic acid (OA) using in vitro and in-silico approaches. The leaf of AS was extracted by soxhlet extraction using n-hexane and methanol. The methanol extract of AS (MEAS) was subjected to GC-MS analysis. Quantification of total phenolic and flavonoid content and OA were carried out by HPLC and HPTLC analysis, respectively. In vitro antioxidant (DPPH, NO, and H2O2) and anti-diabetic (α-amylase and α-glucosidase) potentials of MEAS, OA, and a combination of MEAS and OA (MEAS + OA) were studied at different concentrations using ascorbic acid and acarbose as standard, respectively. An in-silico study determined their binding interactions with α-amylase (PDB ID-1B2Y) and α-glucosidase (PDB ID-3W37). We found that the combination of MEAS + OA exhibited the highest in vitro antioxidant and anti-diabetic activities compared to MEAS and OA. It concluded that OA has a significant role in potentiating the anti-diabetic effect of A. squamosa. GC-MS analysis of MEAS revealed three major bioactives like bicyclo[7.2.0]undec-4- ene, 4,11,11-trimethyl-8-methylene-,[1R-(1R*,4Z,9S*)]-, germacrene D and undecane. The highest amount of phenolic (tannic acid and gallic acid) (150 μg/ml) and flavonoid (rutin and quercetin) (40 μg/ml) compounds were found in MEAS. OA was quantified as 356.74 ng/ml in MEAS by HPTLC. The significant inhibitory effects of MEAS, OA, and (MEAS + OA) on free radicals and α-amylase and α-glucosidase were observed concentration-dependent. However, MEAS + OA exhibited a greater percentage of inhibition than MEAS and OA alone. The in-silico analysis revealed highest docking-score of OA (-9.8 & -8.8), Germacrene D (-7.5 & -6.5) and Bicyclo[ 7.2.0]undec-4-ene, 4,11,11-trimethyl-8-methylene-,[1R-(1R*,4Z,9S*)]-, (-7.0 & -6.4) against IB2Y and 3W37 proteins, respectively.
糖尿病（DM）是由于胰腺β细胞分泌的胰岛素不足或胰岛素抵抗引起的代谢紊乱，其发病率在全球范围内迅速上升。本研究的目的是采用体外和体内方法，评估鳞叶木贼（AS）叶提取物和齐墩果酸（OA）组合的体外抗氧化和抗糖尿病功效。AS 的甲醇提取物（MEAS）进行了 GC-MS 分析。以抗坏血酸和阿卡波糖为标准，分别研究了不同浓度的 MEAS、OA 以及 MEAS 和 OA 组合（MEAS + OA）的体外抗氧化（DPPH、NO 和 H2O2）和抗糖尿病（α-淀粉酶和α-葡萄糖苷酶）潜力。我们发现，与 MEAS 和 OA 相比，MEAS + OA 组合具有最高的体外抗氧化和抗糖尿病活性。对 MEAS 的气相色谱-质谱分析发现了三种主要的生物活性物质，如双环[7.2.0]十一碳-4-烯、4,11,11-三甲基-8-亚甲基-[1R-(1R*,4Z,9S*)]-、胚芽烯 D 和十一烷。酚类化合物（单宁酸和没食子酸）（150 μg/ml）和类黄酮（芦丁和槲皮素）（40 μg/ml）在 MEAS 中含量最高。通过 HPTLC 法，MEAS 中的 OA 定量为 356.74 ng/ml。MEAS、OA和（MEAS + OA）对自由基、α-淀粉酶和α-葡萄糖苷酶的明显抑制作用呈浓度依赖性。不过，MEAS + OA 的抑制率高于 MEAS 和 OA 本身。硅内分析表明，OA（-9.8 和 -8.8）、锗蒽 D（-7.5 和 -6.5）和双环[7.2.0]十一碳-4-烯、4,11,11-三甲基-8-亚甲基-[1R-(1R*,4Z,9S*)]-（-7.0 和 -6.4）分别对IB2Y 和 3W37 蛋白具有最高的对接分数。
{"title":"In vitro and in-silico Anti-diabetic Evaluation of the Combination of\u0000Annona squamosa Linn., Leaf Extract and Oleanolic Acid","authors":"Sasmita Dash, Nityananda Sahoo, G. Pattnaik, Chandan Das, Sovan Pattnaik, Goutam Ghosh, Goutam Rath, B. Kar","doi":"10.2174/0115734072294929240206060527","DOIUrl":"https://doi.org/10.2174/0115734072294929240206060527","url":null,"abstract":"\u0000\u0000Diabetes mellitus (DM) is a metabolic disorder caused by insufficient\u0000insulin production from pancreatic β-cells or insulin resistance; its prevalence rapidly increases\u0000worldwide. Increasing reports indicate that most plant bioactive agents exhibited alternative and\u0000safe effects in managing DM.\u0000\u0000\u0000\u0000The study aims to evaluate the in vitro antioxidant and anti-diabetic efficacy of the\u0000combination of Annona squamosa Linn. (AS) leaf extract and Oleanolic acid (OA) using in vitro\u0000and in-silico approaches.\u0000\u0000\u0000\u0000The leaf of AS was extracted by soxhlet extraction using n-hexane and methanol. The\u0000methanol extract of AS (MEAS) was subjected to GC-MS analysis. Quantification of total phenolic\u0000and flavonoid content and OA were carried out by HPLC and HPTLC analysis, respectively.\u0000In vitro antioxidant (DPPH, NO, and H2O2) and anti-diabetic (α-amylase and α-glucosidase)\u0000potentials of MEAS, OA, and a combination of MEAS and OA (MEAS + OA) were studied at\u0000different concentrations using ascorbic acid and acarbose as standard, respectively. An in-silico\u0000study determined their binding interactions with α-amylase (PDB ID-1B2Y) and α-glucosidase\u0000(PDB ID-3W37).\u0000\u0000\u0000\u0000We found that the combination of MEAS + OA exhibited the highest in vitro antioxidant\u0000and anti-diabetic activities compared to MEAS and OA. It concluded that OA has a significant\u0000role in potentiating the anti-diabetic effect of A. squamosa.\u0000\u0000\u0000\u0000GC-MS analysis of MEAS revealed three major bioactives like bicyclo[7.2.0]undec-4-\u0000ene, 4,11,11-trimethyl-8-methylene-,[1R-(1R*,4Z,9S*)]-, germacrene D and undecane. The highest\u0000amount of phenolic (tannic acid and gallic acid) (150 μg/ml) and flavonoid (rutin and quercetin)\u0000(40 μg/ml) compounds were found in MEAS. OA was quantified as 356.74 ng/ml in MEAS\u0000by HPTLC. The significant inhibitory effects of MEAS, OA, and (MEAS + OA) on free radicals\u0000and α-amylase and α-glucosidase were observed concentration-dependent. However, MEAS +\u0000OA exhibited a greater percentage of inhibition than MEAS and OA alone. The in-silico analysis\u0000revealed highest docking-score of OA (-9.8 & -8.8), Germacrene D (-7.5 & -6.5) and Bicyclo[\u00007.2.0]undec-4-ene, 4,11,11-trimethyl-8-methylene-,[1R-(1R*,4Z,9S*)]-, (-7.0 & -6.4) against\u0000IB2Y and 3W37 proteins, respectively.\u0000","PeriodicalId":10772,"journal":{"name":"Current Bioactive Compounds","volume":"9 8","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-02-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139962957","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
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